Design and synthesis of novel 2,4-diaryl-5H-indeno[1,2-b]pyridine derivatives, and their evaluation of topoisomerase inhibitory activity and cytotoxicity

Title
Design and synthesis of novel 2,4-diaryl-5H-indeno[1,2-b]pyridine derivatives, and their evaluation of topoisomerase inhibitory activity and cytotoxicity
Author(s)
이응석타라만카다얏박찬미[박찬미]전규연[전규연]틸바하두르다빠마가르비스트가네쉬유한영권영주[권영주]
Keywords
DNA TOPOISOMERASES; 2,4,6-TRISUBSTITUTED PYRIDINE; 2,4,6-TRIPHENYL PYRIDINES; I INHIBITION; MOIETY; POTENT; 2,4-DIARYL; TARGETS; CELLS
Issue Date
201501
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Citation
BIOORGANIC & MEDICINAL CHEMISTRY, v.23, no.1, pp.160 - 173
Abstract
For the development of potential anticancer agents, we designed and synthesized 30 new 2,4-diaryl-5H-indeno[1,2-b]pyridine derivatives containing aryl moiety such as furyl, thienyl, pyridyl, and phenyl at 2- and 4-position of 5H-indeno[1,2-b]pyridine. They were evaluated for topoisomerase I and II inhibitory activity, and cytotoxicity against several human cancer cell lines. Among prepared 30 compounds, 7, 8, 9, 10, 12, 14, 16, 19, 20, 22, and 23 with 2- or 3-furyl and/or 2- or 3-thienyl either at 2- or 4-position of central pyridine showed the significant or moderate topoisomerase II inhibitory activity. Compounds 7, 8, 11, 12, 13, and 22 with 2-furyl, 2-thienyl or 3-thienyl at 2-position of central pyridine showed the significant or moderate topoisomerase I inhibitory activity. Especially, compound 12 with strong topoisomerase II inhibitory activity at 100 mu M and 20 mu M, and moderate topoisomerase I inhibitory activity displayed strong cytotoxicity against several human cancer cell lines. (C) 2014 Elsevier Ltd. All rights reserved.
URI
http://hdl.handle.net/YU.REPOSITORY/33750http://dx.doi.org/10.1016/j.bmc.2014.11.010
ISSN
0968-0896
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약학대학 > 약학부 > Articles
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